Bis(phenylsulfonyl)sulfide as a Bifunctional Single‐Sulfur Source for the Rapid Assembly of Unsymmetric Diaryl Sulfides Enabled by Copper Catalyst

Abstract Rapid access to unsymmetrical diaryl sulfides through a bifunctional single‐sulfur source is a very attractive strategy. Here we report the utilization of bis(phenylsulfonyl)sulfide as a bielectrophilic sulfide platform molecule for chemoselective and sequential installation of two different aryl nucleophiles by twice copper‐catalyzed Chan–Lam‐type cross couplings to access diverse unsymmetrical diaryl sulfides. This strategy demonstrates good tolerance to a wide range of aryl boronic acids under different metal catalysts, good functional group compatibility, as well as the extension to the modification of complex bioactive molecules.